67469-75-4

67469-75-4 structure

Name: GBR 12783 dihydrochloride
Chemical Name: 1-[2-(Diphenylmethoxy)ethyl]-4-[(2E)-3-phenyl-2-propen-1-yl]piper azine dihydrochloride
CAS Number: 67469-75-4
Molecular Formula: C₂₈H₃₄Cl₂N₂O
Molecular Weight: 485.48800
Catalog: Signaling Pathways GPCR/G Protein Dopamine Receptor
Create Date: 2019-01-14 10:28:51
Modify Date: 2024-01-30 11:51:01
GBR 12783 dihydrochloride is a specific, potent and selective dopamine uptake inhibitor that inhibits the [3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 dihydrochloride can improve memory performance and increase hippocampal acetylcholine release in rats[1][2].

Name	1-[2-(Diphenylmethoxy)ethyl]-4-[(2E)-3-phenyl-2-propen-1-yl]piper azine dihydrochloride
Synonyms	2,9,10(1H)-Anthracenetrione,6-ethyl-4,5-dihydroxy-1,1,3,7-tetramethyl Kenpaullone garvatin B quinone

Description	GBR 12783 dihydrochloride is a specific, potent and selective dopamine uptake inhibitor that inhibits the [3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 dihydrochloride can improve memory performance and increase hippocampal acetylcholine release in rats[1][2].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor Research Areas >> Neurological Disease
In Vivo	GBR 12783 (10 mg/kg; intraperitoneal injection; for 100 minutes; male Sprague-Dawley rats) treatment reinforces specifically dopamine transmission only at synapses instantaneously active, increases hippocampal ACh release and improves memory performance in a passive avoidance task[1]. Animal Model: Male Sprague-Dawley rats (180-200 g)[1] Dosage: 10 mg/kg Administration: Intraperitoneal injection; for 100 minutes Result: For a moderate electric shock intensity (0.4 mA), improveed retention performance, increased hippocampal acetylcholine release in vivo.
References	[1]. Nail-Boucherie K, et al. The specific dopamine uptake inhibitor GBR 12783 improves learning of inhibitory avoidance and increases hippocampal acetylcholine release. Brain Res Cogn Brain Res. 1998 Oct;7(2):203-5. [2]. Bonnet JJ, et al. GBR 12783, a potent and selective inhibitor of dopamine uptake: biochemical studies in vivo and ex vivo. Eur J Pharmacol. 1986 Feb 18;121(2):199-209.

Hazard Codes	Xi

18903-01-0

32669-06-0

~49%

67469-75-4

Literature: Van Der Zee; Koger; Gootjes; Hespe European Journal of Medicinal Chemistry, 1980 , vol. 15, # 4 p. 363 - 370